Composite Emulsion Coating for Small-Intestine Release
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Solution Overview
Problem
Existing coating systems fail to provide controlled release of active ingredients in the gastrointestinal tract, particularly after passing the stomach, leading to undesired release locations.
Innovation Solution
A coating system comprising an aqueous solution with a gum having emulsifying properties and an oily phase with a solid oil and enteric coating material, such as Candelilla wax, is used to create a delayed release mechanism in the small intestine.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If a conventional coating system is used, then the particle can be coated with a protective layer, but the active ingredient is released in the wrong location (not in the small intestine)
Solution Approach 1:
The coating system uses a composite emulsion comprising an aqueous phase with gum (emulsifying agent) and an oily phase with enteric coating material and solid oil. This composite structure creates a coating that remains intact in the stomach's acidic environment but dissolves in the small intestine, achieving precise spatial control of drug release.
Solution Approach 2:
The invention exploits parameter changes in the gastrointestinal tract, specifically the change in pH and enzymatic environment from stomach to small intestine. The enteric coating material is designed to resist dissolution at stomach pH but dissolve at the higher pH and enzymatic conditions of the small intestine, enabling location-specific release.
2Reliability
If the coating system uses only enteric coating material, then delayed release is achieved, but the coating may not form a stable emulsion
Solution Approach 1:
The gum acts as an intermediary substance with emulsifying properties. It stabilizes the emulsion by forming a protective interface between the aqueous and oily phases, preventing separation while allowing the enteric coating material to perform its delayed release function. The gum's emulsifying action ensures homogeneous distribution of the coating components.
Solution Approach 2:
The gum serving as an emulsifying agent performs multiple functions: it stabilizes the emulsion structure, aids in forming a uniform coating layer, and does not interfere with the enteric properties of the coating material. This multi-functionality simplifies the overall formulation while achieving both stability and delayed release.
3Ease of manufacture
If the oily phase uses liquid oil only, then the emulsion is easy to form, but the coating does not provide sufficient delayed release
Solution Approach 1:
The oily phase is formulated as a composite mixture of liquid oil and solid oil. The liquid oil facilitates emulsion formation and maintains flexibility, while the solid oil provides the necessary rigidity and delayed release properties. This composite approach combines the advantages of both oil types.
Solution Approach 2:
The inclusion of solid oil changes the physical parameters of the oily phase, increasing its viscosity and solid content. This modification enhances the coating's ability to resist dissolution in the stomach while maintaining emulsifiability during the coating process, achieving both ease of manufacture and reliable delayed release.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The coating system ensures controlled release of active ingredients in the small intestine, achieving delayed release where desired, enhancing targeted delivery.
Implementation Method 1
an (i) aqueous solution comprising a. water, and b. at least one gum having emulsifying properties
Implementation Method 2
an (ii) oily phase comprising a. at least one enteric coating material
Implementation Method 3
b. at least one oil, which is solid at 20° C.
Data Source
AI summary
The present invention relates to a new coating system useful for coating particles, which comprise an active ingredient. Such coated particles, when consumed, do show a controlled release in the human or animal body.